Peer-review started: September 29, 2014
First decision: October 21, 2014
Revised: December 9, 2014
Accepted: December 18, 2014
Article in press: December 19, 2014
Published online: March 28, 2015
Processing time: 236 Days and 17.2 Hours
Since disability in multiple sclerosis (MS) is a product of neurodegeneration and deficient remyelination, the ability to enhance neuroregeneration and myelin regeneration in MS is an enticing goal for MS drug development. In particular, remyelination treatments could promote return of neurological function and also prevent further axonal loss and neurodegeneration in MS due to trophic effects of myelin. The study of remyelination has advanced dramatically in the last several years such that a number of pathways inhibiting remyelination have been discovered, including those involving LINGO-1, Notch-1, hyaluronan, retinoid X receptor, and wnt/ß-catenin. Other approaches such as high throughput drug screening for remyelination drugs have caught fire, with identification of dozens of known drugs with oligodendrocyte maturation stimulatory effects. Several drugs identified through screens and other mechanisms are in the process of being further evaluated for remyelination in MS and MS models. We discuss the potential molecular targets and the variety of mechanisms towards drug identification and development in remyelination for MS.
Core tip: Over the last several years numerous remyelination pathways important to multiple sclerosis (MS) have been identified, including those of LINGO-1, hyaluronan, Notch-1, retinoid X receptor receptor, and wnt/ß-catenin. Newer discoveries include the pathways involving Chemokine (C-X-C Motif) ligand 12/C-X-C chemokine receptor type 4 and G protein-coupled receptor 17, and the involvement of Endothelin-1 in the Notch pathway. High-throughput screens have identified multiple antimuscarinic drugs with good remyelination. Also identified by screens, clemastine, with similar antimuscarinic but also antihistamine effects, may be useful in remyelination in MS. Drug repurposing, through screens or more serendipitously, has found that many drugs could enhance remyelination, including benztropine, clemastine, quetiapine, fasudil, olesoxime, and ibudilast, among others.